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1. 发明专利

JP2011252004A Diaminopyrimidines as p2x3 and p2x2/3 antagonists 有权
标题翻译：作为P2X3和P2X2 / 3拮抗剂的二氨基嘧啶
公开(公告)号：JP2011252004A
公开(公告)日：2011-12-15
申请号：JP2011172873
申请日：2011-08-08
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： CARTER DAVID SCOTT , DILLON MICHAEL PATRICK , HAWLEY RONALD CHARLES , LIN CLARA JEOU JEN , PARISH DANIEL WARREN , BROKA CHRIS ALLEN , JAHANGIR ALAM
IPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61P7/12 , A61P13/02 , A61P13/06 , A61P13/08 , A61P13/10 , A61P25/04 , A61P25/06 , A61P29/00 , A61P43/00 , C07D239/49 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D239/49 , A61K31/505 , A61K31/506 , C07D239/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide a compound and method for treatment of diseases mediated by P2Xand/or P2X/receptor antagonists.SOLUTION: This invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, solvate or prodrug thereof. In the formula (I), D is an optional oxygen; X is -CH2- or the like; Y is hydrogen, -NRdRe or the like; Ris alkyl, alkenyl or the like; R, R, Rand Reach independently is hydrogen, alkyl or the like; Ris hydrogen, alkyl or the like; and one of Rand Ris hydrogen, and the other thereof is hydrogen, alkyl or the like. The method for treatment of the diseases includes administering to a subject in need an effective amount of a compound (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof.
摘要翻译：要解决的问题：提供用于治疗由P2X 3 和/或P2X 2 / 3 受体拮抗剂。解决方案：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或前药。在式（I）中，D是任选的氧; X是-CH 2 - 等; Y是氢，-NRdRe等; R 1是烷基，链烯基等; R 2 ，R 3 ，R 4 ，R 5 各自独立地为氢，烷基等; R 6是氢，烷基等; 并且R 7 和R 8之一是氢，另一个是氢，烷基等。治疗疾病的方法包括向有需要的受试者施用有效量的化合物（I）或其药学上可接受的盐，溶剂合物或前药。版权所有（C）2012，JPO＆INPIT

2. 发明专利

JP2014193906A Diaminopyrimidine as p2x3 and p2x2/3 antagonist 有权
标题翻译：二氨基嘧啶作为P2X3和P2X2 / 3拮抗剂
公开(公告)号：JP2014193906A
公开(公告)日：2014-10-09
申请号：JP2014115301
申请日：2014-06-03
申请人： F. Hoffmann-La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： CARTER DAVID SCOTT , DILLON MICHAEL PATRICK , HAWLEY RONALD CHARLES , LIN CLARA JEOU JEN , PARISH DANIEL WARREN , BROKA CHRIS ALLEN , JAHANGIR ALAM
IPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/538 , A61P1/04 , A61P9/10 , A61P13/02 , A61P13/08 , A61P13/10 , A61P25/04 , A61P25/06 , A61P31/04 , A61P31/12 , A61P33/00 , A61P39/02 , A61P43/00 , C07D239/49 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D239/49 , A61K31/505 , A61K31/506 , C07D239/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide a compound and method for treating a disease mediated by P2Xand/or P2Xreceptor antagonists.SOLUTION: A compound is represented by the formula (I). In the formula, D is optionally oxygen, X is -CH2-; -O-; or the like, Y is hydrogen; or -N, R, R, R, R, R, R, Rand Rare selected from hydrogen; alkyl; alkenyl; cycloalkyl; cycloalkenyl; halo; haloalkyl; hydroxyalkyl; or the like.
摘要翻译：要解决的问题：提供用于治疗由P2X和/或P2X受体拮抗剂介导的疾病的化合物和方法。溶液：化合物由式（I）表示。在该式中，D任选为氧，X为-CH 2 - ; -O-; 等等，Y是氢; 或-N，R，R，R，R，R，R，R 3选自氢; 烷基; 烯基; 环烷基; 环烯基; 光环; 卤代; 羟; 或类似物。

3. 发明专利

JP2011126899A Diaminopyrimidine as p2x3 and p2x2/3 antagonist 有权
标题翻译：二氨基嘧啶作为P2X3和P2X2 / 3拮抗剂
公开(公告)号：JP2011126899A
公开(公告)日：2011-06-30
申请号：JP2011033729
申请日：2011-02-18
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： CARTER DAVID SCOTT , DILLON MICHAEL PATRICK , HAWLEY RONALD CHARLES , LIN CLARA JEOU JEN , PARISH DANIEL WARREN , BROKA CHRIS ALLEN , JAHANGIR ALAM
IPC分类号： C07D239/49 , A61K31/505 , A61K31/506 , A61K31/538 , A61P9/10 , A61P13/08 , A61P13/10 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P29/00 , A61P39/02 , A61P43/00 , C07D239/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D239/49 , A61K31/505 , A61K31/506 , C07D239/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide a new P2X 3 and/or P2X 2/3 receptor antagonists, and to provide a therapeutic agent for treatment of genitourinary disease or a disease associated with pain using the same. SOLUTION: There is provided a compound expressed by formula (I), or a pharmaceutically acceptable salt, solvate or prodrug thereof (wherein X is -CH 2 -, -O-, -CHOH-, -S(O) n -, or -NR c -; n is 0-2; R c is H or alkyl; Y is H or -NR d R e ; either one of R d and R e is H, and the other is H, alkyl, cycloalkyl or the like). COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供新的P2X SB3和/或P2XS2 / 3S / SB>受体拮抗剂，并提供用于治疗泌尿生殖系疾病或与使用其相关的疼痛相关的疾病。提供由式（I）表示的化合物或其药学上可接受的盐，溶剂合物或前药（其中X为-CH 2 S，-O - ， - CHOH- ，-S（O）n - ， - 或-NR S - ， - n为0-2; R b为H或烷基; Y 是H或-NR SB，其中R SB和R SB之一是H，并且另一个是H，烷基，环烷基等）。版权所有（C）2011，JPO＆INPIT

4. 发明申请

WO2009153178A2 ARYL KETONE AS MRI 审中-公开
标题翻译： ARYL KETONE作为MRI
公开(公告)号：WO2009153178A2
公开(公告)日：2009-12-23
申请号：PCT/EP2009056985
申请日：2009-06-08
申请人： HOFFMANN LA ROCHE , IYER PRAVIN , LIN CLARA JEOU JEN , LUCAS MATTHEW C , LYNCH STEPHEN M , MADERA ANN MARIE , OZBOYA KEREM EROL , SCHOENFELD RYAN CRAIG , WEIKERT ROBERT JAMES
发明人： IYER PRAVIN , LIN CLARA JEOU JEN , LUCAS MATTHEW C , LYNCH STEPHEN M , MADERA ANN MARIE , OZBOYA KEREM EROL , SCHOENFELD RYAN CRAIG , WEIKERT ROBERT JAMES
IPC分类号： C07D207/08 , C07D211/32 , C07D401/10 , C07D403/06 , C07D405/06 , C07D451/02
CPC分类号： C07D207/08 , C07D211/32 , C07D401/10 , C07D403/06 , C07D405/06 , C07D451/02 , C07D487/04
摘要： This invention pertains to aryl pyrrolidinyl and piperidinyl ketone compounds of formula (I) wherein R1 and R2 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, and methods for using the same. In particular, compounds of the present invention are useful for treatment of diseases associated with monoamine reuptake inhibition.
摘要翻译：本发明涉及其中R 1和R 2如本文所述的式（I）的芳基吡咯烷基和哌啶基酮化合物及其药学上可接受的盐和酯，及其使用方法。特别地，本发明的化合物可用于治疗与单胺再摄取抑制有关的疾病。

5. 发明专利

MY186650A HETEROARYL PYRROLIDINYL AND PIPERIDINYL KETONE DERIVATIVES 未知
公开(公告)号：MY186650A
公开(公告)日：2021-08-03
申请号：MYPI20092331
申请日：2007-12-11
申请人： HOFFMANN LA ROCHE
发明人： IYER PRAVIN , LUCAS MATTHEW C , MADERA ANN MARIE , WEIKERT ROBERT JAMES , LIN CLARA JEOU JEN , LYNCH STEPHEN M , OZBOYA KEREM EROL , SCHOENFELD RYAN CRAIG
IPC分类号： A61K31/4523 , C07D401/06 , C07D205/04 , C07D207/08 , C07D211/30 , C07D401/10 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C07D451/02 , C07D487/04
摘要： Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n. Ar. R', R2 . R' and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds. (No suitable figure)

7. 发明专利

BRPI0907885A2 Compostos antiviras hetrocíclicos 未知
公开(公告)号：BRPI0907885A2
公开(公告)日：2015-07-21
申请号：BRPI0907885
申请日：2009-02-05
申请人： HOFFMANN LA ROCHE
发明人： LABADIE SHARADA SHENVI , LIN CLARA JEOU JEN , TALAMAS FRANCISCO XAVIER , WEIKERT ROBERT JAMES
IPC分类号： C07D307/84 , A61K31/343 , A61P31/14 , C07D407/04 , C07D407/12 , C07D413/04 , C07D413/12 , C07D417/04

8. 发明专利

AR082154A1 DERIVADOS DE PIRAZOLO[1,5-a]PIRIMIDINA COMO MODULADORES DE IRAK4 未知
公开(公告)号：AR082154A1
公开(公告)日：2012-11-14
申请号：ARP110102497
申请日：2011-07-12
申请人： HOFFMANN LA ROCHE
发明人： LUCAS MATTHEW C , HERMANN JOHANNES CORNELIUS , KUGLSTATTER ANDREAS , ARORA NIDHI , CHEN SHAOQING , PAPP EVA , TALAMAS FRANCISCO XAVIER , LABADIE SHARADA SHENVI , LIN CLARA JEOU JEN , WANNER JUTTA , ZHAI YANSHENG , MOORE AMY GERALDINE
IPC分类号： C07D487/04 , A61K31/4365 , A61K31/519 , A61P11/00 , A61P29/00 , C07D495/04
摘要： Los compuestos en cuestión son útiles para el tratamiento de estados patológicos mediados por las IRAK.Reivindicación 1: Un compuesto de la fórmula (1) o de la fórmula (2) o una sal farmacéuticamente aceptable de los mismos, en las que X es N o CH; m es el número 1 ó 2; Ar es: arilo opcionalmente sustituido; o heteroarilo opcionalmente sustituido; R1 es: hidrógeno; alquilo C1-6; alcoxi C1-6; hidroxi; hidroxi-alquilo C1-6; alquilamino C1-6; amino-alquilo C1-6; amino-alquilamino C1-6; hidroxi-alquilamino C1-6; cicloalquilamino C3-6; amino-cicloalquilamino C3-6; amino-heterocicloalquilamino C3-6; aminocarbonilo; halógeno; hidroxi-alquilo C1-6 o hidroxi-alcoxi C1-6; y R2 es: hidrógeno; o alquilo C1-6.

9. 发明专利

MY145465A DIAMINOPYRIMIDINES AS P2X3 AND P2X2/3 ANTAGONISTS. 未知
公开(公告)号：MY145465A
公开(公告)日：2012-02-15
申请号：MYPI20050871
申请日：2005-03-03
申请人： HOFFMANN LA ROCHE
发明人： CARTER DAVID SCOTT , DILLON MICHAEL PATRICK , HAWLEY RONALD CHARLES , LIN CLARA JEOU JEN , PARISH DANIEL WARREN , BROKA CHRIS ALLEN , JAHANGIR ALAM
IPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： COMPOUNDS AND METHODS FOR TREATING DISEASES MEDIATED BY A P2X₃ AND/OR A P2X₂/₃ RECEPTOR ANTAGONIST, THE METHODS COMPRISING ADMINISTERING TO A SUBJECT IN NEED THEREOF AN EFFECTIVE AMOUNT OF A COMPOUND OF FORMULA (&Igr;) OR A PHARMACEUTICALLY ACCEPTABLE SALT, SOLVATE OR PRODRUG THEREOF, WHEREIN D, X, Y, R¹, R², R³, R⁴, R5⁵, R⁶, R⁷ AND R⁸ ARE AS DEFINED HEREIN.

10. 发明专利

CO6190531A2 DERIVADOS DE HETEROARIL-PIRROLIDINIL- Y-PIPERIDINIL-CETONA 未知
公开(公告)号：CO6190531A2
公开(公告)日：2010-08-19
申请号：CO09053154
申请日：2009-05-22
申请人： HOFFMANN LA ROCHE
发明人： IYER PRAVIN , LIN CLARA JEOU JEN , LUCAS MATTHEW C , MADERA ANN MARIE , OZBOYA KEREM EROL , WEIKERT ROBERT JAMES , SCHOENFELD RYAN CRAIG
IPC分类号： A61K31/4523 , C07D205/04 , C07D207/08 , C07D409/06 , C07D487/04
摘要： 1.- Un compuesto de la fórmula I:o una sal farmacéuticamente aceptable del mismo, en la que: m es un número de 0 a 3; n es un número de 0 a 2; Ar es: indolilo opcionalmente sustituido; indazolilo opcionalmente sustituido; azaindolilo opcionalmente sustituido; azaindazolilo opcionalmente sustituido; 2, 3-dihidro-indolilo opcionalmente sustituido; 1,3-dihidro-indol-2-on-ilo opcionalmente sustituido; benzotiofenilo opcionalmente sustituido; bencimidazolilo opcionalmente sustituido; benzoxazolilo opcionalmente sustituido; bencisoxazolilo opcionalmente sustituido; benzotiazolilo opcionalmente sustituido; bencisotiazolilo opcionalmente sustituido; quinolinilo opcionalmente sustituido; 1,2,3,4-tetrahidroquinolinilo opcionalmente sustituido; quinolin-2-on-ilo opcionalmente sustituido; isoquinolinilo opcionalmente sustituido; naftalenilo opcionalmente sustituido; piridinilo opcionalmente sustituido; tiofenilo opcionalmente sustituido; R1 es: alquilo C1-6; alquenilo C2-6; alquinilo C2-6; hetero-alquilo C1-6; halo-alquilo C1-6; halo-alquenilo C2-6; cicloalquilo C3-7; (cicloalquil C3-7) -alquilo C1-6; (alquil C1-6) - (cicloalquil C3-6) -alquilo C1-6; alcoxi C1-6; alquilsulfonilo C1-6; alquilsulfanilo C1-6; arilo opcionalmente sustituido; heteroarilo opcionalmente sustituido; heterociclil-alquilo C1-6; aril-alquilo C1-3, cuya porción arilo está opcionalmente sustituida; heteroaril-alquilo C1-3, cuya porción heteroarilo está opcionalmente sustituida; ariloxi; aril-alcoxi C1-6; heteroariloxi; o heteroaril-alcoxi C1-6; R2 es: hidrógeno; o alquilo C1-6; y Ra y Rb con independencia entre sí son: hidrógeno; alquilo C1-6; alcoxi C1-6; halógeno; hidroxi; o oxo; o Ra y Rb forman, juntos, un alquileno C1-2; con la condición de que cuando m es 1, n es 2 y Ar es fenilo opcionalmente sustituido, entonces R1 no sea metilo ni etilo, y en donde opcionalmente sustituidos significa uno a cuatro sustituyentes, seleccionados de alquilo, cicloalquilo, alcoxi, halógeno, haloalquilo, haloalcoxi, ciano, nitro, heteroalquilo, amino, acilamino, mono-alquilamino, di-alquilamino, hidroxialquilo, alcoxialquilo, benciloxi, cicloalquilalquilo, cicloalcoxi, cicloalquilalcoxi, alquilsulfoniloxi, tiofenilo, pirazolilo, piridinilo, morfolinocarbonilo, -(CH2)q-S(O)rRf; -(CH2)qNRgRh; -(CH2)q-C(=O)-NRgRh; -(CH2)q-C(=O)-C(=O)-NRgRh; -(CH2)q-SO2-NRgRh; -(CH2)q-N(Rf)-C(=O)-Ri; -(CH2)q-C(=O)-Ri; o -(CH2)q-N(Rf)-SO2-Rg, donde q es 0 o 1, r es de 0 a 2, Rf, Rg y Rh cada uno es independientemente hidrógeno o alquilo, y cada R1 es independientemente hidrógeno, alquilo, hidroxi o alcoxi.

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